4-acetamido-2-methyl benzaldehyde | 84257-50-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-acetamido-2-methyl benzaldehyde
• 英文别名: 4-formyl-3-methylacetanilide；N-(4-formyl-3-methylphenyl)acetamide；2-methyl-4-acetamidobenzaldehyde
• CAS: 84257-50-1
• 化学式: C₁₀H₁₁NO₂
• mdl: MFCD11557920
• 分子量: 177.203
• InChiKey: OQWBSIMVDHAYEQ-UHFFFAOYSA-N

物化性质

• 沸点：
  377.7±30.0 °C(Predicted)
• 密度：
  1.177±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  46.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-acetamido-2-methyl benzaldehyde 在 乙酸铵 、 盐酸 、 sodium tetrahydroborate 作用下， 以 乙醇 为溶剂， 反应 12.0h， 生成 1-(4-amino-2-methylphenyl)-2-nitropropane
  参考文献：
  名称：

  Florvall; Persson, Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry, 1982, vol. 36, # 3 B, p. 141 - 146

  摘要：

  DOI：
• 作为产物：
  描述：

  4-乙酰氨基-2-甲基苯甲酸 在 manganese(IV) oxide 、 硼烷四氢呋喃络合物 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 反应 0.37h， 生成 4-acetamido-2-methyl benzaldehyde
  参考文献：
  名称：

  WO2007/144400

  摘要：

  公开号：

文献信息

• Imidazopyridine compounds and processes for preparation thereof
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US04831041A1

  公开（公告）日：1989-05-16

  The invention relates to an imidazopyridine compound of the formula: ##STR1## wherein R.sup.1 is lower alkynyl, lower alkynyloxy(lower)alkyl or N,N-di(lower)alkylamino(lower)alkynyl, R.sup.2 is lower alkyl, R.sup.3 is mono (or di or tri)-phenyl(lower)alkyl substituted by one or more substituent(s) selected from cyano, carbamoyl, mono (or di or tri(phenyl(lower)alkylamino, acylamino, carboxy, esterified carboxy, hydroxy, hydroxy(lower)alkyl, acyloxy(lower)alkyl, acyloxy, mono (or di or tri)phenyl(lower)alkoxy, lower alkoxy(lower)alkoxy, tetrahydropyranyloxy, and acylamino(lower)alkyl or mono (or di or tri) phenyl(lower)alkyl substituted by lower alkyl and one additional substituent selected from hydroxy(lower)alkyl, amino, N-lower alkyl-N-acylamino, mono (or di or tri)phenyl(lower)alkylamino, acylamino and lower alkylamino, and R.sup.4 is hydrogen or lower alkyl, and a pharmaceutically acceptable salt thereof, useful in the treatment of ulcers.

  该发明涉及一种具有以下结构的咪唑吡啶化合物：##STR1##其中R.sup.1是较低的炔基、较低的炔氧基(较低)烷基或N,N-二(较低)烷基氨基(较低)炔基，R.sup.2是较低的烷基，R.sup.3是被一个或多个来自氰基、氨甲酰基、单(或二或三)苯基(较低)烷基氨基、酰胺基、羧基、酯化羧基、羟基、羟基(较低)烷基、酰氧基(较低)烷基、酰氧基、单(或二或三)苯基(较低)氧基、较低的烷氧(较低)烷氧基、四氢吡喃氧基以及被较低烷基和一个来自羟基(较低)烷基、氨基、N-较低烷基-N-酰氨基、单(或二或三)苯基(较低)烷基氨基、酰胺基和较低烷基氨基的一个额外取代基选择的单(或二或三)苯基(较低)烷基，R.sup.4是氢或较低的烷基，以及其药学上可接受的盐，用于治疗溃疡。
• Studies on Anti-platelet Agents. II. Synthesis and Platelet-Inhibitory Activity of 5-Methyl-4-(3-pyridyl)-2-(substituted Benzimidazol-5-yl)imidazoles.
  作者：Akito TANAKA、Kiyotaka ITO、Shigetaka NISHINO、Yukio MOTOYAMA、Hisashi TAKASUGI

  DOI：10.1248/cpb.42.560

  日期：——

  A series of 5-methyl-4-(3-pyridyl)-2-(substituted benzimidazol-5-yl)imidazole derivatives was synthesized and tested for anti-platelet and vasodilatory activities. Some compounds were found to have potent activities and low acute toxicity. In particular, 5-methyl-4-(3-pyridyl)-2-(7-chloro-6-methoxy-2-methylbenzimidazol-5-yl)imidazole (26) and 5-methyl-4-(3-pyridyl)-2-(7-chloro-3-methoxy-2-methylbenzimidazol-5-yl)imidazole (33) exhibited 63% or 51% inhibition at a dose of 10 mg/kg for anti-patelet activity ex vivo in rats, respectively, while they showed no toxicity even at 180 or 100 mg/kg, respectively. Compound 33 also exhibited potent vasodilatory activity (ED50=11 μg/ml). Enzyme studies on these imidazoles showed that the novel imidazoles inhibit some snzymes which are involved in the platelet aggregation cascade such as cyclooxygenase, phosphodiesterase (PDE), and thromboxane A2 synthetase. The enzyme assay also suggested that the inhibitory activity on PDE may account for the vasodilatory activity of these imidazoles.

  合成了一系列5-甲基-4-(3-吡啶基)-2-(取代苯并咪唑-5-基)咪唑衍生物，并测试了它们的抗血小板和扩血管活性。发现某些化合物具有较强的活性和低急性毒性。特别是，5-甲基-4-(3-吡啶基)-2-(7-氯-6-甲氧基-2-甲基苯并咪唑-5-基)咪唑（26）和5-甲基-4-(3-吡啶基)-2-(7-氯-3-甲氧基-2-甲基苯并咪唑-5-基)咪唑（33）在给药剂量为10 mg/kg时，分别在大鼠的抗血小板活性测试中表现出63%或51%的抑制率，而在180 mg/kg或100 mg/kg时，均未显示出毒性。化合物33还表现出较强的扩血管活性（ED50=11 μg/ml）。对这些咪唑的酶学研究表明，新型咪唑抑制了参与血小板聚集级联反应的一些酶，如环氧合酶、磷酸二酯酶（PDE）和血栓素A2合成酶。酶活性测试还表明，对PDE的抑制活性可能是这些咪唑的扩血管活性的原因。
• [EN] PIPERAZINYL-SULFONAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF GPR38 RECEPTOR MEDIATED DISEASES<br/>[FR] DÉRIVÉS DE PIPÉRAZINYL-SULFONAMIDE UTILES DANS LE TRAITEMENT DE MALADIES INDUITES PAR LE RÉCEPTEUR GPR38
  申请人：GLAXO GROUP LTD

  公开号：WO2009068552A1

  公开（公告）日：2009-06-04

  The present invention relates to novel motilin agonists of formula (IA), processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

  本发明涉及一种新颖的式(I A)的莫替林激动剂，以及其制备方法、含有它们的药物组合物以及它们在治疗各种疾病中的用途。
• Processes for making and using alkylaminoarylcarbonyl compounds
  申请人：Eastman Kodak Company

  公开号：US06124503A1

  公开（公告）日：2000-09-26

  A method of making an alkylaminoarylcarbonyl compound having Formula I: ##STR1## wherein R is an alkyl group; A is an aryl (including heteroaryl) ring; each R' is independently an alkyl group which may form a ring with Z or Z'; p is 0, 1, 2, or 3; each Z, Z', and Y is independently hydrogen or a substituent; and n is 0, 1, or 2; comprising: (a) blocking the carbonyl function of an aminoarylcarbonyl compound via condensation with an active methylene compound (b) alkylating this blocked amniocarbonyl compound via reductive alkylation with an alkyl or aryl (including heteroaryl) carbonyl compound, and (c) deblocking of the blocked alkylaminoarylcarbonyl compound via base hydrolysis to regenerate the carbonyl function and give the desired alkylaminocarbonyl compound.

  一种制备具有式I的烷基氨基芳基羰基化合物的方法：其中，R是烷基；A是芳基（包括杂环芳基）环；每个R'独立地是可以与Z或Z'形成环的烷基；p为0、1、2或3；每个Z、Z'和Y独立地是氢或取代基；n为0、1或2；包括：（a）通过与活性甲基化合物缩合来阻断氨基芳基羰基化合物的羰基功能；（b）通过还原性烷基化与烷基或芳基（包括杂环芳基）羰基化合物烷基化这种阻断的氨基羰基化合物；（c）通过碱水解去除阻断，再生羰基功能并给出所需的烷基氨基羰基化合物。
• Compounds
  申请人：Mitchell Jason Darren

  公开号：US20080027065A1

  公开（公告）日：2008-01-31

  The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.

  本发明涉及式(I)化合物，其制备方法，含有它们的制药组合物以及它们在治疗通过GPR38受体介导的疾病或疾病中的应用。